表面活性剂对无形固体分散的溶液行为和膜传输的影响
Amjad Alhalaweh1, Mira El Sayed2, Lucia Kovac3
1College of Pharmacy, University of Sharjah, Sharjah, United Arab Emirates; Recipharm OT Chemistry AB, SE-754 50 Uppsala, Sweden.
Journal of pharmaceutical sciences
|November 4, 2024
概括
使用TPGS等表面活性剂开发无形固体分散物 (ASD),可增强药物溶解和超和,使难以溶解的化合物过度和. 这种配方策略改善了膜传输和口服生物可用性.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 物理化学 物理化学
背景情况:
- 难以溶解的化合物为口服药物输送提出了配方挑战.
- 无形固体分散 (ASD) 是一种提高可溶性和溶解率的策略.
- 表面活性剂可以提高药物溶解度,调节超和行为.
研究的目的:
- 开发一种不溶性化合物 (AK100) 的无形固体分散 (ASD).
- 研究不同表面活性剂 (SDS,PS80,TPGS) 对AK100溶解,超和膜传输的影响.
- 用计算模型评估溶解度和表面活性剂溶解度之间的关系.
主要方法:
- 确定AK100在不同表面活性剂度的晶体和无形形式中的溶解度.
- 通过溶剂蒸发来制备ASD.
- 使用和不使用表面活性剂的非沉溶解实验.
- 基于Caco-2细胞的膜运输研究.
- 基于活动和基于度的超和比率计算.
主要成果:
- 晶体和无形AK100的溶解度都与表面活性剂度线性增加.
- 与SDS和PS80.0不同,TPGS至少维持了三个小时的超和.
- 与晶体粉相比,ASD配方增强了膜流量,TPGS进一步增加了它.
- 基于活动的超和比率始终高于基于度的比率.
结论:
- 表面活性剂,特别是TPGS,显著改善了来自ASD的AK100的溶解和超和.
- 使用溶解辅助剂的配方增强了药物膜传输.
- 与适当的表面活性剂相结合的ASD技术为改善难溶性药物的口服生物利用性提供了可行的策略.
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